Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Application of composition of benzimidazolyl and 2-chloroethylamino derivatives of guava dialdehyde heteroterpene in preparing anti-inflammatory drugs

A composition and drug technology, applied in the direction of drug combination, anti-inflammatory agent, medical preparations containing active ingredients, etc., can solve the problems of high toxicity and low safety

Inactive Publication Date: 2018-06-22
CHANGZHOU HIGH TECH RES INST OF NANJING UNIV +1
View PDF1 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The existing drugs for the treatment of inflammation have the problems of high toxicity and low safety. It is of great value to find compounds or lead compounds from natural products and carry out structural modification to obtain their derivatives, so as to obtain potential drugs with high efficiency and low toxicity

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Application of composition of benzimidazolyl and 2-chloroethylamino derivatives of guava dialdehyde heteroterpene in preparing anti-inflammatory drugs
  • Application of composition of benzimidazolyl and 2-chloroethylamino derivatives of guava dialdehyde heteroterpene in preparing anti-inflammatory drugs
  • Application of composition of benzimidazolyl and 2-chloroethylamino derivatives of guava dialdehyde heteroterpene in preparing anti-inflammatory drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Example 1 Preparation of a guava dialdehyde heteroterpene

[0013] A preparation method of guava dialdehyde heteroterpenoids (I) refers to the literature published by Meng Shao et al. (MengShao et al., 2010. 12 (2010) 5040–5043) method.

[0014]

Embodiment 2

[0015] Example 2 Synthesis of an O-bromoethyl derivative (II) of guava dialdehyde heteroterpene

[0016] Compound I (474 ​​mg, 1.00 mmol) was dissolved in 20 mL of benzene, tetrabutylammonium bromide (TBAB) (0.16 g), 1,2-dibromoethane (7.520 g, 40.00 mmol) and 12 mL of 50% sodium hydroxide solution. The mixture was stirred at 35 °C for 8 h. After 8 hours, the reaction solution was poured into ice water, extracted twice with dichloromethane immediately, and the organic phase solutions were combined. Then the organic phase solution was washed with water and saturated brine three times successively, then dried with anhydrous sodium sulfate, and finally concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:0.5, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of Compound II (502...

Embodiment 3

[0021] Example 3 Synthesis of O-(benzimidazolyl) ethyl derivative (III) of guava dialdehyde heteroterpene

[0022] Compound II (344mg, 0.5mmol) was dissolved in 25mL of acetonitrile, anhydrous potassium carbonate (690mg, 5.0mmol), potassium iodide (168mg, 1.0mmol) and benzimidazole (4720mg, 40mmol) were added thereto, and the mixture was heated to reflux for 3h . After the reaction was completed, the reaction solution was poured into 20 mL of ice water, extracted three times with an equal amount of dichloromethane, and the organic phases were combined. The combined organic phases were successively washed with water and saturated brine, dried over anhydrous sodium sulfate, and concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:0.5, v / v), the yellow concentrated elution band was collected and the solvent was evaporated to obtain a yello...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses an application of a composition of benzimidazolyl and 2-chloroethylamino derivatives of guava dialdehyde heteroterpene in preparing anti-inflammatory drugs, relates to the fields of organic synthesis and medicinal chemistry, and in particular relates to the composition of benzimidazolyl and 2-chloroethylamino derivatives of guava dialdehyde heteroterpene, a prepariaotn method of the composition, and the application of the composition in preparing the anti-inflammatory drugs. The invention discloses the composition of the benzimidazolyl and 2-chloroethylamino derivativesof guava dialdehyde heteroterpene and the preparation method of the composition. The pharmacological experiment shows that the composition of the benzimidazolyl and 2-chloroethylamino derivatives ofguava dialdehyde heteroterpene has the anti-inflammation effect and has the value of being developed into the anti-inflammatory drugs.

Description

technical field [0001] The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to a composition, a preparation method and an application thereof. Background technique [0002] Inflammation occurs locally but can also affect the whole body. Local clinical features are redness, heat, swelling, pain and dysfunction. Redness and heat are due to the expansion of local blood vessels and the acceleration of blood flow due to inflammation. Swelling is caused by local inflammatory hyperemia and exudation of blood flow components. The development of drugs with anti-inflammatory effects is of great significance for the verification of relief and pain relief. [0003] The existing drugs for the treatment of inflammation have the problems of high toxicity and low safety. It is of great value to find compounds or lead compounds from natural products and carry out structural modification to obtain their derivatives, so as to obtain potential drugs...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K31/4184A61K31/335A61P29/00C07D405/14C07D313/06
CPCA61K31/335A61K31/4184C07D313/06C07D405/14A61K2300/00
Inventor 华子春李媛媛
Owner CHANGZHOU HIGH TECH RES INST OF NANJING UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com